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KPG-121 + abiraterone
- Development stage
- Unknown
- Lead developer
- Kangpu Biopharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
KPG-121 + abiraterone is an investigational oral combination therapy for metastatic castration-resistant prostate cancer (mCRPC). KPG-121 is a novel lenalidomide analogue and CRBN E3 ligase modulator that induces proteasomal degradation of casein kinase 1α (CK1α) and the transcription factors Aiolos (IKZF3) and Ikaros (IKZF1), resulting in antiproliferative, antiangiogenic, and immunomodulatory effects. Abiraterone acetate inhibits CYP17A1, blocking androgen synthesis, contributing to androgen deprivation in prostate cancer. Preclinical and early clinical studies show synergistic antitumor activity when the two agents are combined, with promising efficacy and tolerability observed in phase 1 and ongoing phase 2/3 trials for first-line mCRPC[1][2][4][5][7].
- Other names
- abiraterone acetate
02
Targets
CK1α (Casein kinase I alpha)IKZF1 (Ikaros family zinc finger protein 1)CRBN (Cereblon)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)IKZF3 (Zinc finger protein Aiolos)
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